Synthesis of novel progestin–rhenium conjugates as potential ligands for the progesterone receptor

Wüst, F.; Skaddan, Marc B.; Leibnitz, P.; Spies, Hartmut; Katzenellenbogen, John A.; Johannsen, B.

doi:10.1016/s0968-0896(99)00119-4

Cited by 32 publications

(15 citation statements)

References 20 publications

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“…RBA was also found to depend on the nature of the spacer between the metal chelate and the steroid moiety. Similar observations and tendencies have been reported for the progestin complexes [27]. For both examples, the organometallic cyclopentadienyl-tricarbonyl systems were superior to the dithioether-tricarbonyl systems in terms of RBA for the corresponding receptors.…”

Section: Examples Of Small Molecules Labelled With Tc/re-tricarbonylsupporting

confidence: 84%

Current use and future potential of organometallic radiopharmaceuticals

Schibli

Schubiger

2002

European Journal of Nuclear Medicine and Molecular Imaging

300

256

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Contrary to common belief, organometallic compounds exhibit remarkable stability in aerobic and even diluted aqueous solutions. Technetium-sestamibi (Cardiolite) is one of the most prominent examples of this class of compounds routinely used in nuclear medicine. This review summarises the recent progress in labelling of biomolecules with organometallic complexes for diagnostic and therapeutic application in radiopharmacy and exemplifies in detail developments focussing on organometallic technetium- and rhenium-tricarbonyl technologies. The value of such technologies has been recognised and they have become a valuable alternative to common labelling methodologies. An increasing number of groups have started to employ an organometallic precursor for the purpose of radioactive labelling of various classes of biomolecules, and the advantages and limitations of this new technique are compared with those of other labelling methods. The synthetic access to appropriate precursors via double-ligand exchange or aqueous carbonyl kit preparation for routine application is described. Strategies and examples for the design of appropriate bifunctional chelating agents for the Tc/Re-tricarbonyl core are given. The functionalization of biomolecules such as tracers for the central nervous system (dopaminergic and serotonergic), tumour affine peptides (somatostatin receptors, neuroreceptors) and tumour binding single-chain antibody fragments is summarised. Where possible and appropriate, the in vitro and in vivo results in respect of these examples are compared with those obtained with classical (99m)Tc/(188)Re(V)- and (111)In-labelled analogues. The preclinical results show the in many ways superior characteristics of organometallic labelling techniques.

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Section: Examples Of Small Molecules Labelled With Tc/re-tricarbonylsupporting

confidence: 84%

Current use and future potential of organometallic radiopharmaceuticals

Schibli

Schubiger

2002

European Journal of Nuclear Medicine and Molecular Imaging

300

256

View full text Add to dashboard Cite

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“…The isomer formation influences the specific receptor binding because of the different metal-ligand orientation and may produce labelled species with different affinity for the same target, principally for small biomolecules. [27] From the perspective of developing a new drug, single and chemically stable products are essential for FDA approval.…”

Section: Discussionmentioning

confidence: 99%

Synthesis and Characterisation of [Re(CO)₃(SS)(P)] Complexes: A [2+1] Concept for ^99mTc‐ and ¹⁸⁸Re‐Radiopharmaceutical Applications

et al. 2005

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“…The two enantiomers of the facial Re(CO) 3 Cl-pyta-C 3 N 3 (ref. [63][64][65] were not separated before coupling to the chiral mestranol, resulting in two diastereoisomers. These two diastereoisomers, bearing the same facial Re(CO) 3 Cl-pyta moiety, are expected to show similar IR and luminescence properties.…”

Section: Synthesis and Characterization Ofmentioning

confidence: 99%

Detection of an estrogen derivative in two breast cancer cell lines using a single core multimodal probe for imaging (SCoMPI) imaged by a panel of luminescent and vibrational techniques

Clède

Lambert

Sandt

et al. 2013

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3-Methoxy-17α-ethynylestradiol or mestranol is a prodrug for ethynylestradiol and the estrogen component of some oral contraceptive formulations. We demonstrate here that a single core multimodal probe for imaging - SCoMPI - can be efficiently grafted onto mestranol allowing its tracking in two breast cancer cell lines, MDA-MB-231 and MCF-7 fixed cells. Correlative imaging studies based on luminescence (synchrotron UV spectromicroscopy, wide field and confocal fluorescence microscopies) and vibrational (AFMIR, synchrotron FTIR spectromicroscopy, synchrotron-based multiple beam FTIR imaging, confocal Raman microspectroscopy) spectroscopies were consistent with one another and showed a Golgi apparatus distribution of the SCoMPI-mestranol conjugate in both cell lines.

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Synthesis of novel progestin–rhenium conjugates as potential ligands for the progesterone receptor

Cited by 32 publications

References 20 publications

Current use and future potential of organometallic radiopharmaceuticals

Current use and future potential of organometallic radiopharmaceuticals

Synthesis and Characterisation of [Re(CO)₃(SS)(P)] Complexes: A [2+1] Concept for ^99mTc‐ and ¹⁸⁸Re‐Radiopharmaceutical Applications

Detection of an estrogen derivative in two breast cancer cell lines using a single core multimodal probe for imaging (SCoMPI) imaged by a panel of luminescent and vibrational techniques

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Synthesis of novel progestin–rhenium conjugates as potential ligands for the progesterone receptor

Cited by 32 publications

References 20 publications

Current use and future potential of organometallic radiopharmaceuticals

Current use and future potential of organometallic radiopharmaceuticals

Synthesis and Characterisation of [Re(CO)3(SS)(P)] Complexes: A [2+1] Concept for 99mTc‐ and 188Re‐Radiopharmaceutical Applications

Detection of an estrogen derivative in two breast cancer cell lines using a single core multimodal probe for imaging (SCoMPI) imaged by a panel of luminescent and vibrational techniques

Contact Info

Product

Resources

About

Synthesis and Characterisation of [Re(CO)₃(SS)(P)] Complexes: A [2+1] Concept for ^99mTc‐ and ¹⁸⁸Re‐Radiopharmaceutical Applications